Fatostatin HBr

製品コードS8284 バッチS828401

化学情報

	Synonyms	125B11 HBr	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₈H₁₈N₂S·HBr
	分子量	375.33	CAS No.	298197-04-3
Solubility (25°C)*	体外	Ethanol	58 mg/mL warmed with 50ºC water bath (154.53 mM)
		DMSO	7 mg/mL (18.65 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Fatostatin HBr is an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.
in vitro	Fatostatin inhibits the insulin-induced adipogenesis of 3T3-L1 cells and the serum-independent growth of human androgen-independent prostate cancer (DU145) cells. Fatostatin blocks the activation of SREBPs in cells in tissue culture^[1]. Fatostatin suppresses cell proliferation and anchorage-independent colony formation in both androgen-responsive LNCaP and androgen-insensitive C4-2B prostate cancer cells. Fatostatin also reduced in vitro invasion and migration in both cell lines. Further, fatostatin causes G2/M cell cycle arrest and induces apoptosis by increasing caspase-3/7 activity and the cleavages of caspase-3 and PARP^[2].
in vivo	Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake^[1]. Fatostatin significantly inhibits subcutaneous C4-2B tumor growth and markedly decreases serum PSA level compared to the control group^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CHO-K1 cells
	濃度	20 μM
	反応時間	20 h
	実験の流れ	On day 0, CHO-K1 cells are plated out onto a 96-well plate in medium A. On day 2, the cells are transiently cotransfected with pCMV-PLAP-BP2(513–1141), pCMV-SCAP, and pAc-β-gal, using Lipofectamine reagent. After incubation for 5 hr, the cells are washed with PBS and then incubated in medium B, in the absence or presence of fatostatin (20 μM) or sterols (10 μg/mL cholesterol and 1 μg/mL 25-hydroxycholesterol). After 20 hr of incubation, an aliquot of the medium is assayed for secreted alkaline phosphatase activity. The cells in each well are lysed and used for measurement of β-galactosidase activities. The alkaline phosphatase activity is normalized by the activity of β-galactosidase.
動物実験	動物モデル	Obese (ob/ob) mice (C57BL/6J background)
	投薬量	30 mg/kg
	投与方法	i.p.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

NFYC-37 promotes tumor growth by activating the mevalonate pathway in bladder cancer [ Cell Rep, 2023, 42(8):112963]	PubMed: 37561631
TGF-β1 promotes SCD1 expression via the PI3K-Akt-mTOR-SREBP1 signaling pathway in lung fibroblasts [ Respir Res, 2023, 24(1):8]	PubMed: 36627645
Visualization and quantification of de novo lipogenesis using a FASN-2A-GLuc mouse model [ Ann Transl Med, 2022, 10(18):958]	PubMed: 36267736
Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer [ Nat Cancer, 2021, 2(1):66-82]	PubMed: 33738458
Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer [ Nat Cancer, 2021, 2(1):66-82]	PubMed: 33738458
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4]	PubMed: 34580494
p53 transcriptionally regulates SQLE to repress cholesterol synthesis and tumor growth [ EMBO Rep, 2021, e52537]	PubMed: 34459531
Genetic Screens Identify Host Factors for SARS-CoV-2 and Common Cold Coronaviruses [ Cell, 2020, S0092-8674(20)31626-3]	PubMed: 33333024
Fatostatin in Combination with Tamoxifen Induces Synergistic Inhibition in ER-Positive Breast Cancer [ Drug Des Devel Ther, 2020, 14:3535-3545]	PubMed: 32921987
Staphylococcal Enterotoxin C2 Mutant-Directed Fatty Acid and Mitochondrial Energy Metabolic Programs Regulate CD8+ T Cell Activation [ J Immunol, 2020, 205(8):2066-2076]	PubMed: 32938730

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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